Corosolic Acid

Clinical Overview

Use

Corosolic acid has numerous biological properties, including antidiabetic, anti-inflammatory, antiproliferative, and protein kinase C inhibition activity. However, there is a lack of clinical evidence to support these uses.

Source

History

Corosolic acid has numerous biological properties including antidiabetic, anti-inflammatory, antiproliferative, and protein kinase C inhibition activity.1, 2 It is found in numerous plants species, particularly L. speciosa.3 Most medical research focuses on the compound's efficacy in diabetes. Glucosol (or GlucoFit) is a commercially available product primarily marketed in Japan and the United States as a dietary supplement for weight loss and blood sugar balance.1 Corosolic acid is found in numerous cosmetic products, including creams, lotions, hair tonics, as well as in hypoglycemic health foods.3, 4, 5

Chemistry

Corosolic acid is a naturally occurring pentacyclic triterpene also known as 2 alpha-hydroxy ursolic acid.6, 7 Chemical analyses focus on the study of corosolic acid and its derivatives as inhibitors of glycogen phosphorylases for potential development of antidiabetic agents.1, 6 There is documented commercial interest in improving the chemical production of corosolic acid and its esters.8, 9

Animal data

In a 2-stage Berenblum experiment on mouse skin papillomas, the inhibitory effect of corosolic acid was comparable or equivalent to beta-carotene, rosmarinic acid, and alpha-linolenic acid.12

Diabetes

Corosolic acid may improve the insulin pathway. The action of insulin is mediated by tyrosine phosphorylation and initiated by the binding of insulin to the insulin receptor. Corosolic acid may act as an insulin sensitizer, enhancing insulin receptor B phosphorylation indirectly by inhibiting certain nonreceptor protein tyrosine phosphatases.13 Corosolic acid may also enhance GLUT4 glucose transporter processing of glucose uptake into muscle cells.14 Another study reported that corosolic acid inhibited gluconeogenesis by increasing the production of the gluconeogenic intermediate fructose-2,6-bisphosphate in isolated hepatocytes. Corosolic acid may promote glycolysis.15, 16

Other pharmacologic activity

Chemotherapeutic

Corosolic acid enhanced the activity of treatment with tobramycin against Pseudomonas aeruginosa in a biofilm inhibition assay.23

Inflammation

Activity against the classical pathway of the complement system is documented for corosolic acid.24

Metabolic syndrome

In an animal model on metabolic syndrome, corosolic acid had antihypertensive, lipid-lowering, antioxidant, and anti-inflammatory effects on rats.25 In a similar study, corosolic acid reduced blood pressure and serum-free fatty acid levels in rats.26

Obesity

There is in vitro evidence for corosolic acid inhibiting protein tyrosine phosphatase 1B; inhibition of this phosphatase is proposed as a therapy for obesity.27 Corosolic acid is also a pancreatic lipase inhibitor, the main enzyme for lipid absorption.28 In a mouse study, corosolic acid acted as a peroxisome proliferator-activated receptor alpha agonist, regulating lipid metabolism and increasing fatty acid beta-oxidation in the liver.29

Pregnancy / Lactation

Avoid use. Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

Counsel patients with diabetes or those taking diabetic medications about the potential additive effects if they are self-medicating with any corosolic oral dietary supplement.

Adverse Reactions

Avoid use with hypersensitivity to any source plants for corosolic acid. Because the product may be derived from several plant species, there is a potential for skin rashes.

A case of severe acute lactic acidosis was attributed to the likely accumulation of corosolic acid in a patient with type 2 diabetes mellitus, gouty arthritis, and stage 3a chronic kidney disease with non-steroidal anti-inflammatory drug (NSAID)-induced acute renal impairment. The patient had been taking corosolic acid daily for 1 month. One week prior to admission, acute NSAID-induced renal hypoperfusion was thought to have occurred after the patient self-medicated with diclofenac for joint pains, which led to a subsequent accumulation of corosolic acid. Corosolic acid has been shown to inhibit gluconeogenesis and enhance glycolysis.33

Disclaimer

This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs. This information should not be used to decide whether or not to take this product. This information does not endorse this product as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this product. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this product. This information is not specific medical advice and does not replace information you receive from your health care provider. You should talk with your health care provider for complete information about the risks and benefits of using this product.

This product may adversely interact with certain health and medical conditions, other prescription and over-the-counter drugs, foods, or other dietary supplements. This product may be unsafe when used before surgery or other medical procedures. It is important to fully inform your doctor about the herbal, vitamins, mineral or any other supplements you are taking before any kind of surgery or medical procedure. With the exception of certain products that are generally recognized as safe in normal quantities, including use of folic acid and prenatal vitamins during pregnancy, this product has not been sufficiently studied to determine whether it is safe to use during pregnancy or nursing or by persons younger than 2 years of age.